Phosphoglycerate Kinase (PGK) Inhibitor
-
PGK1-IN-1
0 ImagesPGK1-IN-1 (Compound 6e) is a potent and selective PGK1 inhibitor (IC50: 33 nM). PGK1-IN-1 inhibits PGK1-mediated glycolytic metabolism and reduces glucose consumption/lactate production. PGK1-IN-1 enhances Nrf2 accumulation and HO-1 expression, and suppresses the transcription and protein levels of the inflammatory cytokines IL-1β and IL-6. PGK1-IN-1 ameliorates Dextran sulfate sodium (DSS) (HY-116282C)-induced experimental colitis in mice. PGK1-IN-1 can be used for research of inflammatory bowel disease (IBD).
-
Ilicicolin H
0 ImagesCat. No.: HY-N8540CAS No.: 12689-26-8Ilicicolin H is a selective and non-ATP-competitive phosphoglycerate kinase 1 (PGK1) (IC50 = 9.02 μM) and mitochondrial cytochrome bc1 reductase (IC50 = 2-3 ng/mL) inhibitor. Ilicicolin H directly binds to PGK1 with KD of 60 μM .Ilicicolin H can inhibit cell proliferation and induce apoptosis. Ilicicolin H can inhibit the lactate production and glucose uptake of hepatocellular carcinoma (HCC) cells. Ilicicolin H has a broad antifungal spectrum including C. albicans, Cryptococcus and A. fumigatus. Ilicicolin H can be used for the researches of cancer and infection, such as hepatocellular carcinoma (HCC) and C. albicans infection.
-
PGK1-IN-3
0 ImagesCat. No.: HY-184191CAS No.: 1185003-32-0PGK1-IN-3 is an orally active PGK1 inhibitor with human PGK1 IC50 values of 0.48 μM and human PGK1 Kd of 63 nM. PGK1-IN-3 binds to the ADP-binding pocket of PGK1, inhibits glycolysis, and reduces glucose consumption and lactate production. PGK1-IN-3 can be used for the research of pancreatic cancer.
-
PGK1-IN-2
0 ImagesCat. No.: HY-178989CAS No.: 3054148-68-1PGK1-IN-2 (Compound 60) is a PGK1 inhibitor with an IC50 of 8.24 μM. PGK1-IN-2 demonstrates a significant ability to inhibit the proliferation of osteosarcoma cells. PGK1-IN-2 interferes with the glycolytic pathway of tumor cells by inhibiting PGK1. PGK1-IN-2 inhibits cell migration and invasion, and induces cell S phase and G2-M phase cycle arrest. PGK1-IN-2 may kill cells by inducing cuproptosis. PGK1-IN-2 shows a significant anti-tumor effect in the MNNG-HOS osteosarcoma xenograft mouse model. PGK1-IN-2 can be used for the study of osteosarcoma.
-
DC-PGKI
0 ImagesCat. No.: HY-177944CAS No.: 2829198-49-2DC-PGKI is an orally active ATP-competitive PGK1 inhibitor(IC50 = 0.16 Μm, Kd = 99.08 nM). DC-PGKI stabilizes PGK1 in vitro and in vivo, and suppresses both glycolytic activity and the kinase function of PGK1. DC-PGKI-mediated inhibition of PGK1 leads to the accumulation of NRF2 (nuclear factor-erythroid factor 2-related factor 2, NFE2L2), which then translocates to the nucleus, binds to the proximal regions of IL-1β and IL-6 genes, and suppresses the LPS-induced expression of these genes. DC-PGKI can be used for the study of colitis.
